期刊
PHARMACEUTICAL RESEARCH
卷 34, 期 5, 页码 1067-1082出版社
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-017-2117-3
关键词
amphotericinB; Candida albicans; chitosan; micro-platelets
资金
- Fondation de Cooperation Scientifique, University Paris Saclay [2014-1127]
Pourpose The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. Methods Micro-platelets were obtained by mixing oleoyl chitosan and alpha-cyclodextrin in water. The formulation is specifically-engineered for mucosal application by dispersing chitosan micro-platelets into thermosensitive pluronic(A (R)) F127 20 wt% hydrogel. Results The formulation completely cured C. albicans vaginal infection in mice and had a superior activity in comparison with AmB-DOC without addition of chitosan micro-platelets. In vitro studies showed that the platelets significantly enhance AmB-DOC antifungal activity since the IC50 and the MIC90 decrease 4.5 and 4.8-times. Calculation of fractional inhibitory concentration index (FICI = 0.198) showed that chitosan micro-platelets act in a synergistic way with AmB-DOC against C. albicans. No synergy is found between spherical nanoparticles composed poly(isobutylcyanoacrylate)/chitosan and AmB-DOC. Conclusion These results demonstrate for the first time the ability of flattened chitosan micro-platelets to have synergistic activity with AmB-DOC against C. albicans candidiasis and highlight the importance of rheological and mucoadhesive behaviors of hydrogels in the efficacy of the treatment.
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